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Highly selective substitutions in 2,3-dichloropyrazine. A novel general approach to aloisines |
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| Authors: | Dmitriy S. Chekmarev Sergey V. Shorshnev Alexander N. Kasatkin |
| Affiliation: | a ChemBridge Corporation, Malaya Pirogovskaya 1, Build. 5, 119435 Moscow, Russia b M.V. Lomonosov Moscow State Academy of Fine Chemical Technology, Prospekt Vernadskogo 86, 119571 Moscow, Russia |
| Abstract: | A highly efficient synthesis of the potent CDKs (cyclin-dependent kinases) inhibitors, aloisines (substituted 5H-pyrrolo[2,3-b]pyrazines) is presented. The method is based on highly selective monosubstitution of a single chlorine atom in 2,3-dichloropyrazine with lithiated ketones, esters, and nitriles followed by co-cyclization of the resulting intermediates with primary amines or hydrazines. |
| Keywords: | 2,3-Dichloropyrazine Aloisines Substituted 5H-pyrrolo[2,3-b]pyrazines α-Arylation Cross-coupling reactions Cyclization |
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